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BMS-509744
CAS No. 439575-02-7
BMS-509744 ( PD 0332991 )
产品货号. M21885 CAS No. 439575-02-7
BMS-509744 是一种有效的、选择性的 ATP 竞争性 Itk 抑制剂，IC50 为 19 nM。
纯度: >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| 规格 | 价格/人民币 | 库存 | 数量 |
| 2MG | ￥947 | 有现货 |
|
| 25MG | ￥7942 | 有现货 |
|
| 50MG | ￥10323 | 有现货 |
|
| 100MG | ￥15570 | 有现货 |
|
| 500MG | 获取报价 | 有现货 |
|
| 1G | 获取报价 | 有现货 |
|
生物学信息
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产品名称BMS-509744
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注意事项本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断
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产品简述BMS-509744 是一种有效的、选择性的 ATP 竞争性 Itk 抑制剂，IC50 为 19 nM。
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产品描述BMS-509744 reduces T-cell receptor-induced functions including PLCγ1 tyrosine phosphorylation, calcium mobilization, IL-2 secretion, and T-cell proliferation in vitro in both human and mouse cells. BMS-488516 and BMS-509744 potently inhibit Itk in vitro with IC50 values of 96 and 19 nM, respectively. Both compounds exhibit competitive kinetics with respect to ATP, suggesting that they bind to the ATP binding site of the Itk kinase domain.
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体外实验BMS-509744 reduces T-cell receptor-induced functions including PLCγ1 tyrosine phosphorylation, calcium mobilization, IL-2 secretion, and T-cell proliferation in vitro in both human and mouse cells. BMS-488516 and BMS-509744 potently inhibit Itk in vitro with IC50 values of 96 and 19 nM, respectively. Both compounds exhibit competitive kinetics with respect to ATP, suggesting that they bind to the ATP binding site of the Itk kinase domain.
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体内实验BMS-509744 and BMS-488516 suppress the production of IL-2 induced by anti-T-cell receptor antibody administered to mice. BMS-509744 exhibits a 50% inhibitory capacity when dosed at 50 mg/kg, irrespective of the amount of induction antibody. BMS-509744 also significantly diminishes lung inflammation in a mouse model of ovalbumin-induced allergy/asthma.
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同义词PD 0332991
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通路Angiogenesis
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靶点CDK
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受体MAPK/DYRK1A
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研究领域——
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适应症——
化学信息
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CAS Number439575-02-7
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分子量447.53
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分子式C??H??N?O?
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纯度>98% (HPLC)
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溶解度DMSO : 5 mg/mL (11.17 mM; ultrasonic and adjust pH to 3 with HCl)；H2O : 0.1 mg/mL (0.22 mM; Need ultrasonic)
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SMILESO=C1C(C(C)=O)=C(C2=CN=C(N=C2N1C3CCCC3)NC4=CC=C(N5CCNCC5)C=N4)C
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化学全称——
运输与储存
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储存条件(-20℃)
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运输条件With Ice Pack
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稳定性≥ 2 years
参考文献
1. Fry DW, et al. Specific inhibition of cyclin-dependent kinase 4/6 by PD 0332991 and associated antitumor activity in human tumor xenografts. Mol Cancer Ther. 2004 Nov;3(11):1427-38.
2. Katsumi Y, et al. Sensitivity of malignant rhabdoid tumor cell lines to PD 0332991 is inversely correlated with p16 expression. Biochem Biophys Res Commun, 2011, 413(1), 62-68.
3. Goel S, et al. CDK4/6 inhibition triggers anti-tumour immunity. Nature. 2017 Aug 24;548(7668):471-475.
产品手册
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